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Synthesis and Antibacterial Activity of N-[2-[5-(Methylthio)Thiophen-2-Yl]-2-Oxoethyl] and N-[2-[5-(Methylthio)Thiophen-2-Yl]-2-(Oxyimino)Ethyl]Piperazinylquinolone Derivatives Publisher Pubmed



Foroumadi A1, 4 ; Oboudiat M2 ; Emami S3 ; Karimollah A2 ; Saghaee L2 ; Moshafi MH4 ; Shafiee A1
Authors
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Authors Affiliations
  1. 1. Faculty of Pharmacy, Pharmaceutical Sciences Research Center, Tehran University of Medical Sciences, Tehran, 14174, Iran
  2. 2. Department of Medicinal Chemistry, Faculty of Pharmacy, Esfahan University of Medical Sciences, Esfahan, Iran
  3. 3. Department of Medicinal Chemistry, Faculty of Pharmacy, Mazandaran University of Medical Sciences, Sari, Iran
  4. 4. Faculty of Pharmacy, Kerman University of Medical Sciences, Kerman, Iran

Source: Bioorganic and Medicinal Chemistry Published:2006


Abstract

A number of N-substituted piperazinylquinolone derivatives were synthesized and evaluated for antibacterial activity against Gram-positive and Gram-negative bacteria. Preliminary results indicated that most compounds tested in this study demonstrated comparable or better activity against Staphylococcus aureus and Staphylococcus epidermidis than their parent piperazinylquinolones as reference drugs. Among these derivatives, ciprofloxacin derivative 5a, containing N-[2-[5-(methylthio)thiophen-2-yl]-2-oxoethyl] residue, showed significant improvement of potency against staphylococci, maintaining Gram-negative coverage. © 2006 Elsevier Ltd. All rights reserved.
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